BR112020004500A2 - derivados de imidazo [1,5-a] pirazina como inibidores de pi3kdelta - Google Patents

derivados de imidazo [1,5-a] pirazina como inibidores de pi3kdelta Download PDF

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Publication number
BR112020004500A2
BR112020004500A2 BR112020004500-4A BR112020004500A BR112020004500A2 BR 112020004500 A2 BR112020004500 A2 BR 112020004500A2 BR 112020004500 A BR112020004500 A BR 112020004500A BR 112020004500 A2 BR112020004500 A2 BR 112020004500A2
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Brazil
Prior art keywords
compound
cancer
optionally substituted
ring
fact
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BR112020004500-4A
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English (en)
Portuguese (pt)
Inventor
Jing Li
Haibo Zhao
Zhiwei Wang
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Beigene, Ltd.
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Publication of BR112020004500A2 publication Critical patent/BR112020004500A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
BR112020004500-4A 2017-09-08 2018-09-07 derivados de imidazo [1,5-a] pirazina como inibidores de pi3kdelta BR112020004500A2 (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN2017101058 2017-09-08
CNPCT/CN2017/101058 2017-09-08
CN2017119373 2017-12-28
CNPCT/CN2017/119373 2017-12-28
CN2018086555 2018-05-11
CNPCT/CN2018/086555 2018-05-11
PCT/CN2018/104559 WO2019047915A1 (en) 2017-09-08 2018-09-07 IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3KDELTA INHIBITORS

Publications (1)

Publication Number Publication Date
BR112020004500A2 true BR112020004500A2 (pt) 2020-12-01

Family

ID=65633578

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112020004500-4A BR112020004500A2 (pt) 2017-09-08 2018-09-07 derivados de imidazo [1,5-a] pirazina como inibidores de pi3kdelta

Country Status (21)

Country Link
US (3) US11220506B2 (fi)
EP (2) EP3679042B1 (fi)
JP (1) JP7128264B2 (fi)
KR (1) KR20200052297A (fi)
CN (2) CN111051312A (fi)
AU (2) AU2018328569B2 (fi)
BR (1) BR112020004500A2 (fi)
CA (1) CA3072842A1 (fi)
DK (1) DK3679042T3 (fi)
ES (1) ES2944658T3 (fi)
FI (1) FI3679042T3 (fi)
HU (1) HUE061898T2 (fi)
IL (1) IL272988B (fi)
MX (1) MX2020002630A (fi)
NZ (1) NZ761680A (fi)
PL (1) PL3679042T3 (fi)
PT (1) PT3679042T (fi)
SG (1) SG11202001286SA (fi)
TW (2) TW202336010A (fi)
WO (1) WO2019047915A1 (fi)
ZA (1) ZA202000875B (fi)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3551630A4 (en) 2016-12-07 2020-07-15 Beigene, Ltd. IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3KDELTA INHIBITORS
TW202336010A (zh) 2017-09-08 2023-09-16 英屬開曼群島商百濟神州有限公司 咪唑並[1 5 A]吡嗪衍生物作爲PI3Kδ抑制劑
TW202313617A (zh) * 2021-05-27 2023-04-01 英屬開曼群島商百濟神州有限公司 PI3Kδ抑制劑的鹽、其晶型、製備方法及用途
IL311402A (en) * 2021-09-14 2024-05-01 Beigene Ltd A method for treating cancer by combining btk inhibitors with pi3 kinase inhibitors

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005089352A (ja) * 2003-09-16 2005-04-07 Kissei Pharmaceut Co Ltd 新規なイミダゾ[1,5−a]ピラジン誘導体、それを含有する医薬組成物およびそれらの用途
AU2004282219C1 (en) * 2003-10-15 2009-12-17 Osi Pharmaceuticals, Inc. Imidazo [1, 5 - a] pyrazine tyrosine kinase inhibitors
US7659274B2 (en) * 2006-01-25 2010-02-09 Osi Pharmaceuticals, Inc. Unsaturated mTOR inhibitors
US20120077813A1 (en) 2009-04-15 2012-03-29 Astrazeneca Ab Imidazole Substituted Pyrimidines Useful in the Treatment of Glycogen Synthase Kinase-3 Related Disorders such as Alzheimer's Disease
KR101792837B1 (ko) * 2009-04-16 2017-11-02 푼다시온 센트로 나시오날 드 인베스티가시오네스 온콜로기카스 카를로스Ⅲ 키나아제 억제제로서 사용을 위한 이미다조피라진
CN103476767B (zh) * 2011-02-09 2015-06-10 弗·哈夫曼-拉罗切有限公司 作为pi3激酶抑制剂的杂环化合物
ES2588186T3 (es) * 2012-01-10 2016-10-31 Bayer Intellectual Property Gmbh Imidazopirazinas sustituidas como inhibidores de la quinasa Akt
MX2020009849A (es) 2012-11-01 2021-09-13 Infinity Pharmaceuticals Inc Tratamiento de canceres utilizando moduladores de las isoformas de pi3 cinasa.
RU2019134551A (ru) 2013-05-30 2019-11-22 Инфинити Фармасьютикалз, Инк. Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы
WO2015058084A1 (en) * 2013-10-18 2015-04-23 Medivation Technologies, Inc. Heterocyclic compounds and methods of use
HRP20211813T1 (hr) * 2014-08-11 2022-03-04 Acerta Pharma B.V. Terapeutske kombinacije inhibitora btk i inhibitora bcl-2
AR102220A1 (es) * 2015-10-08 2017-02-15 Incyte Corp Imidazopiridinas e imidazopirazinas como inhibidores de lsd1
BR112018075999A2 (pt) * 2016-06-16 2019-04-02 Janssen Pharmaceutica Nv derivados de piridina, pirazina e pirimidina bicíclicos como inibidores de pi3k beta
EP3551630A4 (en) * 2016-12-07 2020-07-15 Beigene, Ltd. IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3KDELTA INHIBITORS
TW202336010A (zh) 2017-09-08 2023-09-16 英屬開曼群島商百濟神州有限公司 咪唑並[1 5 A]吡嗪衍生物作爲PI3Kδ抑制劑

Also Published As

Publication number Publication date
PL3679042T3 (pl) 2023-09-04
CN111704615B (zh) 2023-02-17
EP3679042A1 (en) 2020-07-15
ZA202000875B (en) 2021-07-28
JP7128264B2 (ja) 2022-08-30
FI3679042T3 (fi) 2023-05-15
IL272988A (en) 2020-04-30
AU2018328569B2 (en) 2023-07-27
AU2018328569A1 (en) 2020-02-27
ES2944658T3 (es) 2023-06-23
JP2020534259A (ja) 2020-11-26
US20220081447A1 (en) 2022-03-17
CN111704615A (zh) 2020-09-25
HUE061898T2 (hu) 2023-08-28
MX2020002630A (es) 2020-07-20
US11905294B2 (en) 2024-02-20
CA3072842A1 (en) 2019-03-14
EP3679042A4 (en) 2021-01-13
TWI817956B (zh) 2023-10-11
AU2023254925A1 (en) 2023-11-16
KR20200052297A (ko) 2020-05-14
CN111051312A (zh) 2020-04-21
US20200207774A1 (en) 2020-07-02
WO2019047915A1 (en) 2019-03-14
US11220506B2 (en) 2022-01-11
SG11202001286SA (en) 2020-03-30
TW201920116A (zh) 2019-06-01
EP4219502A1 (en) 2023-08-02
IL272988B (en) 2022-08-01
PT3679042T (pt) 2023-05-18
NZ761680A (en) 2023-03-31
TW202336010A (zh) 2023-09-16
DK3679042T3 (da) 2023-05-01
EP3679042B1 (en) 2023-03-01
US20240150361A1 (en) 2024-05-09

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